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WO2003070182A3 - Bloqueurs de canaux sodium - Google Patents

Bloqueurs de canaux sodium Download PDF

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Publication number
WO2003070182A3
WO2003070182A3 PCT/US2003/004817 US0304817W WO03070182A3 WO 2003070182 A3 WO2003070182 A3 WO 2003070182A3 US 0304817 W US0304817 W US 0304817W WO 03070182 A3 WO03070182 A3 WO 03070182A3
Authority
WO
WIPO (PCT)
Prior art keywords
sodium channel
channel blockers
present
variety
treatment
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US2003/004817
Other languages
English (en)
Other versions
WO2003070182A2 (fr
Inventor
Michael R Johnson
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27752677&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2003070182(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority to KR1020107027168A priority Critical patent/KR101225201B1/ko
Priority to EP03742810A priority patent/EP1485360B1/fr
Priority to US10/532,110 priority patent/US20060142306A1/en
Priority to AU2003211135A priority patent/AU2003211135B2/en
Priority to HK05103365.6A priority patent/HK1070369B/en
Priority to KR1020107027167A priority patent/KR101183274B1/ko
Application filed by Individual filed Critical Individual
Priority to JP2003569142A priority patent/JP4557550B2/ja
Priority to SI200332076T priority patent/SI1485360T1/sl
Priority to DK03742810.9T priority patent/DK1485360T3/da
Priority to ES03742810T priority patent/ES2374130T3/es
Priority to KR1020047012934A priority patent/KR101008728B1/ko
Priority to CA2476430A priority patent/CA2476430C/fr
Priority to AT03742810T priority patent/ATE520674T1/de
Publication of WO2003070182A2 publication Critical patent/WO2003070182A2/fr
Publication of WO2003070182A3 publication Critical patent/WO2003070182A3/fr
Anticipated expiration legal-status Critical
Priority to US12/179,353 priority patent/US8198286B2/en
Priority to US13/492,711 priority patent/US8846688B2/en
Priority to US14/158,441 priority patent/US20140179625A1/en
Priority to US14/727,189 priority patent/US20150376146A1/en
Priority to US15/336,574 priority patent/US10167266B2/en
Priority to US16/181,230 priority patent/US20190241528A1/en
Ceased legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
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    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C07D241/28Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
    • C07D241/30Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms in which said hetero-bound carbon atoms are part of a substructure —C(=X)—X—C(=X)—X— in which X is an oxygen or sulphur atom or an imino radical, e.g. imidoylguanidines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C07D241/28Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
    • C07D241/30Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms in which said hetero-bound carbon atoms are part of a substructure —C(=X)—X—C(=X)—X— in which X is an oxygen or sulphur atom or an imino radical, e.g. imidoylguanidines
    • C07D241/32(Amino-pyrazinoyl) guanidines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26Acyclic or carbocyclic radicals, substituted by hetero rings

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  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Immunology (AREA)
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  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Toxicology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Otolaryngology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

L'invention concerne des bloqueurs de canaux sodium ainsi qu'une pluralité de méthodes de traitement utilisant lesdits bloqueurs de canaux de sodium de l'invention.
PCT/US2003/004817 2002-02-19 2003-02-19 Bloqueurs de canaux sodium Ceased WO2003070182A2 (fr)

Priority Applications (19)

Application Number Priority Date Filing Date Title
CA2476430A CA2476430C (fr) 2002-02-19 2003-02-19 Bloqueurs de canaux sodium
ES03742810T ES2374130T3 (es) 2002-02-19 2003-02-19 Bloqueantes de los canales de sodio.
US10/532,110 US20060142306A1 (en) 2002-02-19 2003-02-19 Sodium channel blockers
AU2003211135A AU2003211135B2 (en) 2002-02-19 2003-02-19 Sodium channel blockers
HK05103365.6A HK1070369B (en) 2002-02-19 2003-02-19 Sodium channel blockers
KR1020107027167A KR101183274B1 (ko) 2002-02-19 2003-02-19 나트륨 채널 차단제
EP03742810A EP1485360B1 (fr) 2002-02-19 2003-02-19 Bloqueurs de canaux sodium
JP2003569142A JP4557550B2 (ja) 2002-02-19 2003-02-19 ナトリウムチャネル遮断薬
SI200332076T SI1485360T1 (sl) 2002-02-19 2003-02-19 Blokatorji natrijevih kanalov
DK03742810.9T DK1485360T3 (da) 2002-02-19 2003-02-19 Natriumkanalblokkere
KR1020047012934A KR101008728B1 (ko) 2002-02-19 2003-02-19 나트륨 채널 차단제
KR1020107027168A KR101225201B1 (ko) 2002-02-19 2003-02-19 나트륨 채널 차단제
AT03742810T ATE520674T1 (de) 2002-02-19 2003-02-19 Natriumkanalblocker
US12/179,353 US8198286B2 (en) 2002-02-19 2008-07-24 Sodium channel blockers
US13/492,711 US8846688B2 (en) 2002-02-19 2012-06-08 Sodium channel blockers
US14/158,441 US20140179625A1 (en) 2002-02-19 2014-01-17 Sodium channel blockers
US14/727,189 US20150376146A1 (en) 2002-02-19 2015-06-01 Sodium channel blockers
US15/336,574 US10167266B2 (en) 2002-02-19 2016-10-27 Sodium channel blockers
US16/181,230 US20190241528A1 (en) 2002-02-19 2018-11-05 Sodium channel blockers

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US10/076,571 US6858615B2 (en) 2002-02-19 2002-02-19 Phenyl guanidine sodium channel blockers
US10/076,571 2002-02-19

Related Parent Applications (2)

Application Number Title Priority Date Filing Date
US10/076,571 Continuation-In-Part US6858615B2 (en) 2002-02-19 2002-02-19 Phenyl guanidine sodium channel blockers
US10/076,571 Continuation US6858615B2 (en) 2002-02-19 2002-02-19 Phenyl guanidine sodium channel blockers

Related Child Applications (3)

Application Number Title Priority Date Filing Date
US10532110 A-371-Of-International 2003-02-19
US10/532,110 A-371-Of-International US20060142306A1 (en) 2002-02-19 2003-02-19 Sodium channel blockers
US12/179,353 Continuation US8198286B2 (en) 2002-02-19 2008-07-24 Sodium channel blockers

Publications (2)

Publication Number Publication Date
WO2003070182A2 WO2003070182A2 (fr) 2003-08-28
WO2003070182A3 true WO2003070182A3 (fr) 2003-12-24

Family

ID=27752677

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2003/004817 Ceased WO2003070182A2 (fr) 2002-02-19 2003-02-19 Bloqueurs de canaux sodium

Country Status (13)

Country Link
US (15) US6858615B2 (fr)
EP (1) EP1485360B1 (fr)
JP (2) JP4557550B2 (fr)
KR (3) KR101183274B1 (fr)
AT (1) ATE520674T1 (fr)
AU (2) AU2003211135B2 (fr)
CA (1) CA2476430C (fr)
CY (1) CY1112906T1 (fr)
DK (1) DK1485360T3 (fr)
ES (1) ES2374130T3 (fr)
PT (1) PT1485360E (fr)
SI (1) SI1485360T1 (fr)
WO (1) WO2003070182A2 (fr)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7956059B2 (en) 2004-08-18 2011-06-07 Parion Sciences, Inc. Aliphatic amide and ester pyrazinoylguanidine sodium channel blockers
US8008494B2 (en) 2004-08-18 2011-08-30 Parion Sciences, Inc. Soluble amide and ester pyrazinoylguanidine sodium channel blockers
US8431579B2 (en) 2003-08-18 2013-04-30 Parion Sciences, Inc. Capped pyrazinoylguanidine sodium channel blockers
US9586910B2 (en) 2011-06-27 2017-03-07 Parion Sciences, Inc. 3,5-diamino-6-chloro-N-(N-(4-(4-(2-(hexyl(2,3,4,5,6-pentahydroxyhexyl)amino)ethoxy)phenyl)butyl)carbamimidoyl)pyrazine-2-carboxamide
US9586911B2 (en) 2013-12-13 2017-03-07 Parion Sciences, Inc. Arylalkyl- and aryloxyalkyl-substituted epthelial sodium channel blocking compounds
US9593084B2 (en) 2012-12-17 2017-03-14 Parion Sciences, Inc. Chloro-pyrazine carboxamide derivatives with epithelial sodium channel blocking activity
US9695134B2 (en) 2012-12-17 2017-07-04 Parion Sciences, Inc. 3,5-diamino-6-chloro-N-(n-(4-phenylbutyl)carbamimidoyl)pyrazine-2-carboxamide compounds

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6858615B2 (en) * 2002-02-19 2005-02-22 Parion Sciences, Inc. Phenyl guanidine sodium channel blockers
US6858614B2 (en) * 2002-02-19 2005-02-22 Parion Sciences, Inc. Phenolic guanidine sodium channel blockers
US6903105B2 (en) * 2003-02-19 2005-06-07 Parion Sciences, Inc. Sodium channel blockers
CA2534568A1 (fr) * 2003-08-18 2005-03-24 Parion Sciences, Inc. Bloqueurs du canal sodique a base de pyrazinoylguanidine alaphatique
JP2007502829A (ja) * 2003-08-18 2007-02-15 パリオン・サイエンシィズ・インコーポレーテッド 環状ピラジノイルグアニジンナトリウムチャネルブロッカー
US20050090505A1 (en) * 2003-08-18 2005-04-28 Johnson Michael R. Methods of reducing risk of infection from pathogens
US7745442B2 (en) * 2003-08-20 2010-06-29 Parion Sciences, Inc. Methods of reducing risk of infection from pathogens
CN1882353B (zh) * 2003-11-19 2011-04-20 明治制果株式会社 催涎剂和混合该催涎剂的口腔用组合物以及食品组合物
GB0403864D0 (en) * 2004-02-20 2004-03-24 Ucl Ventures Modulator
EP1789049A4 (fr) * 2004-08-18 2009-07-22 Michael R Johnson Bloqueurs des canaux sodiques a base d'amide cyclique et d'ester pyrazinoylguanidine
US20070021439A1 (en) * 2005-07-25 2007-01-25 Parion Sciences, Inc. Methods of reducing risk of infection from pathogens with soluble amide and ester pyrazinoylguanidine sodium channel blockers
US7807834B2 (en) * 2005-08-03 2010-10-05 Parion Sciences, Inc. Capped pyrazinoylguanidine sodium channel blockers
AU2012201188B2 (en) * 2005-08-03 2013-02-07 Parion Sciences, Inc. New capped pyrazinoylguanidine sodium channel blockers
GB0526244D0 (en) 2005-12-22 2006-02-01 Novartis Ag Organic compounds
US20110195973A1 (en) * 2006-06-09 2011-08-11 Parion Sciences, Inc. Cyclic substituted pyrazinoylguanidine sodium channel blockers possessing beta agonist activity
WO2007146867A2 (fr) * 2006-06-09 2007-12-21 Parion Sciences Inc. Bloqueurs de canaux sodiques pyrazinoylguanidine aliphatiques dotés d'une activité agoniste bêta
PT2035004E (pt) * 2006-06-09 2012-11-21 Parion Sciences Inc Bloqueadores dos canais de sódio de pirazinoilguanidona substituída com fenilo que possuem actividade agonista beta
EP2059239A4 (fr) * 2006-09-07 2010-07-07 Parion Sciences Inc Hydratation de muqueuse et clairance de muqueuse améliorées par traitement avec bloqueurs de canal sodique et osmolytes
MX2009002602A (es) * 2006-09-07 2009-05-28 Parion Sciences Inc Metodos para aumentar la hidratacion mucosa y el despeje mucoso mediante tratamiento con bloqueadores de canal de sodio y osmolitos.
EP1939173A1 (fr) * 2006-12-21 2008-07-02 Pharmeste S.r.l. Dérivés d'urée dibenzyl o-substituée ou de thiourée fonctionnant comme antagonistes du récepteur trpv1
US20080293740A1 (en) * 2007-04-03 2008-11-27 Parion Sciences, Inc. Method of treating acid-sensing ion channel mediated pain, cough suppression, and central nervous system disorders
WO2008124491A1 (fr) * 2007-04-03 2008-10-16 Parion Sciences, Inc. Composes de pyrazinoylguanidine destines a etre utilises en tant que modulateurs de gout
CA2702094C (fr) 2007-10-10 2018-05-01 Parion Sciences, Inc. Administration d'osmolytes par canule nasale
NZ585789A (en) * 2007-12-10 2012-03-30 Novartis Ag Pyrazine-2-carboxamide derivatives to treat diseases mediated by blockade of the epithelial sodium channel
AU2009246799B2 (en) * 2008-02-26 2014-02-27 Parion Sciences, Inc. Poly aromatic pyrazinoylguanidine sodium channel blockers
US20100074881A1 (en) * 2008-07-11 2010-03-25 Parion Sciences, Inc. Multiple nebulizer systems
WO2011081937A1 (fr) 2009-12-15 2011-07-07 Gilead Sciences, Inc. Composés de type corticostéroïde-bêta-agoniste-antagoniste muscarinique pour applications thérapeutiques
US8367829B2 (en) 2010-05-10 2013-02-05 Gilead Sciences, Inc. Bi-functional pyrazolopyridine compounds
AU2011253203A1 (en) 2010-05-10 2012-11-22 Gilead Sciences, Inc. Bifunctional quinoline derivatives
WO2011156355A1 (fr) * 2010-06-09 2011-12-15 Kainos Medicine, Inc. Procédé de production de sels de phénylguanidine et de leurs intermédiaires
CA2819635A1 (fr) 2010-12-01 2012-06-07 Spinal Modulation, Inc. Administration dirigee d'agents a une anatomie neuronale
US8945605B2 (en) 2011-06-07 2015-02-03 Parion Sciences, Inc. Aerosol delivery systems, compositions and methods
WO2012170677A1 (fr) 2011-06-07 2012-12-13 Parion Sciences, Inc. Procédés de traitement
ES2633177T3 (es) 2011-06-27 2017-09-19 Parion Sciences, Inc. Dipéptido química y metabólicamente estable que presenta una potente actividad bloqueadora de los canales de sodio
EA201990616A3 (ru) 2012-05-29 2019-12-30 Парион Сайэнс, Инк. Дендримероподобные аминоамиды, обладающие активностью блокаторов натриевых каналов, для лечения сухости глаз и других заболеваний слизистых оболочек
ES2674665T3 (es) * 2012-12-17 2018-07-03 Parion Sciences, Inc. Compuestos de 3,5-diamino-6-cloro-N-(N-(4-fenilbutilo)carbamimidoilo)-pirazina-2-carboxamida
WO2015007517A1 (fr) 2013-07-15 2015-01-22 Boehringer Ingelheim International Gmbh Nouveaux composés de benzimidazolium tétra-substitués et penta-substitués
JP6461134B2 (ja) * 2013-07-15 2019-01-30 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規ベンゾイミダゾリウム化合物
HK1223561A1 (zh) 2013-08-23 2017-08-04 帕里昂科学公司 二巯基化物类粘液溶解剂
UY36034A (es) 2014-03-18 2015-09-30 Astrazeneca Ab Derivados de 3,5-diamino-6-cloro-pirazina-2-carboxamida y sales farmaceuticamente aceptables de estos
US20150376145A1 (en) 2014-06-30 2015-12-31 Parion Sciences, Inc. Stable sodium channel blockers
JP6826038B2 (ja) 2015-01-30 2021-02-03 パリオン・サイエンシィズ・インコーポレーテッド 新規モノチオール粘液溶解剤
EP3244893A4 (fr) * 2015-02-18 2019-01-09 Parion Sciences, Inc. Bloqueurs de canaux sodiques pour le traitement de troubles de la peau
JP2018520986A (ja) 2015-04-30 2018-08-02 パリオン・サイエンシィズ・インコーポレーテッド ジチオール粘液溶解剤の新規なプロドラッグ
GB201610854D0 (en) 2016-06-21 2016-08-03 Entpr Therapeutics Ltd Compounds
GB201619694D0 (en) 2016-11-22 2017-01-04 Entpr Therapeutics Ltd Compounds
GB201717051D0 (en) 2017-10-17 2017-11-29 Enterprise Therapeutics Ltd Compounds
GB201808093D0 (en) 2018-05-18 2018-07-04 Enterprise Therapeutics Ltd Compounds

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3313813A (en) * 1962-10-30 1967-04-11 Merck & Co Inc (3-amino-5, 6-disubstituted-pyrazinoyl) guanidines
US3573306A (en) * 1969-03-05 1971-03-30 Merck & Co Inc Process for preparation of n-substituted 3,5-diamino-6-halopyrazinamides

Family Cites Families (348)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3268406A (en) 1961-10-12 1966-08-23 Merck & Co Inc Compositions and method of using (3-amino-pyrazinoyl) guanidines
DK109779C (da) 1962-10-30 1968-07-01 Merck & Co Inc Fremgangsmåde til fremstilling af 3-aminopyrazinamidoguanidinforbindelser eller syreadditionssalte heraf.
NL6409714A (fr) 1962-10-30 1965-10-01
US3316266A (en) 1964-03-31 1967-04-25 Merck & Co Inc 3-aminopyrazinoic acid derivatives and process for their preparation
NL6409716A (fr) 1962-10-30 1965-10-01
NL299929A (fr) 1962-10-30
US3274191A (en) 1963-11-15 1966-09-20 Merck & Co Inc N-(3-aminopyrazinoyl) benzamidines and process for preparing
US3240780A (en) 1963-12-23 1966-03-15 Merck & Co Inc Amino-pyrazinoyl guanidines
DE1245967B (de) 1964-03-31 1967-08-03 Merck &. Co., Inc., Rahway, N.J. (V. St. A.) Verfahren zur Herstellung von S.S-Diamino-o-chlor-pyrazincarbonsäurealkylestern
NL6501301A (fr) 1964-04-03 1965-10-04
US3249610A (en) 1964-09-08 1966-05-03 Merck & Co Inc Synthesis of 3-amino, 5-chloro, 6-substituted-pyrazinoates
DE1281818B (de) 1965-07-17 1968-10-31 Rheinische Kalksteinwerke Verfahren zum gleichzeitigen Mahlen mehrerer Rohstoffe unterschiedlicher Mahlbarkeit
US3274192A (en) 1965-10-04 1966-09-20 Merck & Co Inc Derivatives of pyrazine and a method for their preparation
US3341540A (en) 1965-10-04 1967-09-12 Merck & Co Inc 3-amino-6-halopyrazinonitriles and their syntheses
US3361748A (en) 1965-11-22 1968-01-02 Merck & Co Inc Process for the preparation of pteridinones
US3305552A (en) 1965-11-22 1967-02-21 Merck & Co Inc 3-aminopyrazinoic acids and process for their preparation
IL27897A (en) 1966-08-25 1972-02-29 Merck & Co Inc Preparation of pyrazinoalguanides and pyrazinoamidoguanidines
FR1525670A (fr) 1966-08-25 1968-05-17 Merck & Co Inc Procédé de fabrication de guanidines substituées
FR1525671A (fr) 1966-08-25 1968-05-17 Merck & Co Inc Procédé de préparation de (3, 5 - diamino - 6 - halogéno - pyrazinoyl) - guanidines et de (3, 5 - diamino - 6 - halogéno -pyrazinamido) guanidines
NL6707564A (fr) 1966-08-25 1968-02-26
US3660400A (en) 1966-11-17 1972-05-02 Merck & Co Inc Lower alkyl 3-hydroxy and 3-mercaptopyrazinoates
US3472848A (en) 1966-11-17 1969-10-14 Merck & Co Inc 3-hydroxy and 3-mercapto-pyrazinoyl-guanidines,corresponding ethers and thioethers and processes for their preparation
US3527758A (en) 1967-04-13 1970-09-08 Merck & Co Inc Process for the preparation of pyrazinoylguanidines from a pyrazinoic azide and a guanidine
US3507865A (en) 1967-04-27 1970-04-21 Merck & Co Inc 3-hydroxy- and 3-mercaptopyrazinamidoguanidines the corresponding ethers and thioethers and processes for their preparation
US3507866A (en) 1967-08-08 1970-04-21 Merck & Co Inc 1h - imidazo(4,5-b)pyrazin - 2 - one and processes for their preparation
US3487082A (en) 1967-09-28 1969-12-30 Merck & Co Inc 2,4 - diamino - 6 - halopteridines and processes for their preparation
US3503973A (en) 1967-11-07 1970-03-31 Merck & Co Inc Process for preparation of pyrazinoylguanidines
US3515723A (en) 1967-11-14 1970-06-02 Merck & Co Inc 2 - (5 - amino - 1h - 1,2,4 - triazol - 3 - yl)- 3-aminopyrazines and processes for their preparation
US3531484A (en) 1968-02-14 1970-09-29 Merck & Co Inc 1-(3-aminopyrazinoyl)-4,5,5-trisubstituted biguanide products
US3461123A (en) 1968-04-12 1969-08-12 Merck & Co Inc 1h-imidazo(4,5-b)pyrazin-2-ones and processes for their preparation
US3506662A (en) 1968-04-30 1970-04-14 Merck & Co Inc Process for preparation of pyrazinoyland pyrazinamidoguanidines
US3625950A (en) 1968-07-03 1971-12-07 Merck & Co Inc Certain halophenoxy alkanamides, hydrazides and derivatives thereof
US3575975A (en) 1968-07-25 1971-04-20 Merck & Co Inc Process for the preparation of 3-aminopyrazinoylureas
US3539569A (en) * 1968-08-21 1970-11-10 Merck & Co Inc Preparation of pyrazinoylguanidines from pyrazinoylureas
US3544571A (en) 1968-09-04 1970-12-01 Merck & Co Inc Process for making pyrazinoylthiourea compounds
US3555024A (en) 1968-11-13 1971-01-12 Merck & Co Inc 1-(3-aminopyrazinoyl)semicarbazides,1-(3-aminopyrazinoyl) - thiosemicarbazides,and method for their preparation
US3555023A (en) 1968-11-13 1971-01-12 Merck & Co Inc 1-(3 - aminopyrazinoyl) - 3 - substituted-3-thioisosemicarbazides and method for preparation
US3668241A (en) 1968-11-25 1972-06-06 Merck & Co Inc Substituted 1-oxoinden-5-yloxy alkanoic acids
US3586688A (en) 1968-12-18 1971-06-22 Merck & Co Inc Certain aminopyridinecarbonyl guanidines
US3573305A (en) 1968-12-30 1971-03-30 Merck & Co Inc (3-amino-pyrazinoyl)sulfamides and their preparation
US3577418A (en) 1969-02-12 1971-05-04 Merck & Co Inc Pyrazinamide derivatives and processes for their preparation
US3544568A (en) 1969-03-18 1970-12-01 Merck & Co Inc 3-amino-5,6-substituted pyrazinamides
US3660397A (en) 1970-04-17 1972-05-02 Merck & Co Inc Imidazo(4 5-b)pyrazines
US3864401A (en) 1970-12-23 1975-02-04 Merck & Co Inc Substituted 2-aminomethyl-4,6-dihalophenols
US3794734A (en) 1971-03-03 1974-02-26 Merck & Co Inc Methods of treating edema and hypertension using certain 2-aminoethylphenols
US3935313A (en) 1971-03-29 1976-01-27 Jan Marcel Didier Aron-Samuel Pharmaceutical composition containing N-(3-diethyl-aminopropyl)-4-nitro-1-oxide-pyridine-2-carboxamide and process for the treatment of hypertension therewith
US3948895A (en) 1971-09-28 1976-04-06 E. I. Du Pont De Nemours And Company Synthesis of 3,5-diaminopyrazinoic acid from 3,5-diamino-2,6-dicyanopyrazine and intermediates
BE791201A (fr) 1971-11-12 1973-05-10 Merck & Co Inc Indanyloxytetrazoles
US3953476A (en) 1971-12-27 1976-04-27 Merck & Co., Inc. 3-Amino-5-sulfonylbenzoic acids
US3894085A (en) 1972-09-19 1975-07-08 Ciba Geigy Corp New 2-halo nitrones, their manufacture and their use for the manufacture of N-substituted araliphatic aldehyde-nitrones
US3976686A (en) 1972-10-13 1976-08-24 Merck & Co., Inc. [1-Oxo-2,3-hydrocarbylene-5-indanyloxy(or thio)]alkanoic acids
US4085219A (en) 1972-10-13 1978-04-18 Merck & Co., Inc. 1-Oxo-2,2-disubstituted-5-indanyloxy(or thio)alkanoic acids
US3984465A (en) 1972-10-13 1976-10-05 Merck & Co., Inc. 1-Oxo-2,2-disubstituted-5-indanyloxy(or thio)alkanoic acids
US4081554A (en) 1972-10-13 1978-03-28 Merck & Co., Inc. 1-oxo-2,2-disubstituted-5-indanyloxy(or thio)alkano acids
US4091015A (en) 1972-10-27 1978-05-23 American Home Products Corporation 15-Substituted prostanoic acids
US4092356A (en) 1972-10-30 1978-05-30 Merck & Co., Inc. 11,12-Secoprostaglandins
US4066692A (en) 1972-10-30 1978-01-03 Merck & Co., Inc. 11,12-secoprostaglandins
US4055597A (en) 1973-01-26 1977-10-25 Merck & Co., Inc. 10-Aza-11,12-secoprostaglandins
US3987091A (en) 1973-04-12 1976-10-19 Merck & Co., Inc. 11,12-secoprostaglandins
US4033996A (en) 1973-04-25 1977-07-05 Merck & Co., Inc. 8-Aza-9-oxo(and dioxo)-thia-11,12-secoprostaglandins
US4091107A (en) 1973-04-25 1978-05-23 Merck & Co., Inc. 8-Aza-9-oxo(and dioxo)-thia-11,12-secoprostaglandins
US3894065A (en) 1973-04-27 1975-07-08 Merck & Co Inc Aryl-oxo-alkanoic acids
US4177285A (en) 1973-10-11 1979-12-04 Merck & Co., Inc. [1-Oxo-2-thienyl-2-substituted-5-indanyloxy (or thio)]alkanoic acids and derivatives thereof
US4182764A (en) 1973-10-11 1980-01-08 Merck & Co., Inc. Tetrazole derivatives of [1-oxo-2-aryl or thienyl-2-substituted-5-indanyloxy(or thio)]alkanoic acids
US4012524A (en) 1973-10-12 1977-03-15 Merck & Co., Inc. [1-Hydroxy-5-indanyloxy (or thio)]-alkanoic acids
US3929872A (en) 1973-10-12 1975-12-30 Merck & Co Inc Indanacetic acid compounds
US4006180A (en) 1973-10-12 1977-02-01 Merck & Co., Inc. [1,3-Dihydroxy-2-substituted and 2,2-disubstituted-indanyloxy(or thio)]alkanoic acids
US3966966A (en) 1973-10-12 1976-06-29 Merck & Co., Inc. Pharmaceutical compositions and method of treatment employing 1,3-dioxo-2,2-disubstituted indanyloxy alkanoic acids
US3976681A (en) 1973-10-12 1976-08-24 Merck & Co., Inc. [1,3-Dioxo-2-substituted and 2,2-disubstituted- indanyloxy (or thio] alkanoic acids
US4003927A (en) 1973-10-12 1977-01-18 Merck & Co., Inc. (1-Oxo-7,8-disubstituted-1,2,3,4-tetrahydro-6-naphthyloxy)- and (3,4-disubstituted-5-oxo-6,7,8,9-tetrahydro-5H-benzocycloheptene-2-yloxy) acetic acids and derivatives
US3989749A (en) 1973-10-17 1976-11-02 Merck & Co., Inc. 11,12-Secoprostaglandins
US3991087A (en) 1973-12-13 1976-11-09 Merck & Co., Inc. 8-Halo-11,12-secoprostaglandins
US3979361A (en) 1974-02-20 1976-09-07 Merck & Co., Inc. 2-Aminomethyl-6-trihalo-methylphenols
US3914253A (en) 1974-03-04 1975-10-21 Merck & Co Inc 5-Oxo-6-substituted-cyclopent-{8 f{9 -indole-2-carboxylic acids
US3931239A (en) 1974-04-03 1976-01-06 Merck & Co., Inc. 6-Oxo-7-substituted-6H-indeno-[5,4-b]furan(and thiophene)-carboxylic acids
US3958004A (en) 1974-04-23 1976-05-18 Merck & Co., Inc. Phenoxyacetic acid derivatives as uricosuric agents
US3928624A (en) 1974-04-25 1975-12-23 Merck & Co Inc Phenol compounds in treating pain, fever and inflammation
US3956374A (en) 1974-05-03 1976-05-11 Merck & Co., Inc. Aryl-oxo-heptenoic acids
US3974212A (en) 1974-05-22 1976-08-10 Merck & Co., Inc. [1-Hydroximino-2,2-disubstituted-5-indanyloxy-(or thio)]alkanoic acids
AT351182B (de) 1974-06-25 1979-07-10 Merck & Co Inc Verfahren zur herstellung von neuen 9-thia-, 9-oxothia- und 9-dioxothia- 11,12-secoprosta- glandinen
PL98342B1 (pl) 1974-07-30 1978-04-29 Sposob wytwarzania kwasu 1-keto-2-arylo-/lub tienylo/-2-podstawionego-indanyloksy-/lub tio/-5-alkanokarboksylowego
US4020177A (en) 1974-08-30 1977-04-26 Merck & Co., Inc. Substituted phenoxy-tridecanoic acids
US4055596A (en) 1974-09-13 1977-10-25 Merck & Co., Inc. 11,12-Seco-prostaglandins
US3991106A (en) 1974-09-13 1976-11-09 Merck & Co., Inc. 16-Ethers of 8-aza-9-dioxothia-11,12-seco-prostaglandins
US3984552A (en) 1975-02-24 1976-10-05 Merck & Co., Inc. 6-Oxo-7-substituted and 7,7-disubstituted-6H-indeno-[5,4-b]furan (and thiophene) carboxylic acids
JPS51116341A (en) 1975-04-04 1976-10-13 Automob Antipollut & Saf Res Center Detection apparatus for oil pressure
US4018802A (en) 1975-04-09 1977-04-19 Merck & Co., Inc. 9-Thia- and oxothia- and 9-dioxothia-11,12-seco-prostaglandins and processes
US4097504A (en) 1975-04-23 1978-06-27 Merck & Co., Inc. 11,12-Secoprostaglandins
US4092414A (en) 1975-04-25 1978-05-30 Merck & Co., Inc. 3,4-Dihydrospiro-2H-1,3-benzoxazines and their use in treating edema, abnormal electrolyte retention, and inflammation
US4059602A (en) 1975-06-06 1977-11-22 Merck & Co., Inc. 8-Methyl-, phenyl-, or substituted phenyl-11,12-secoprostaglandins
US4059601A (en) 1975-06-06 1977-11-22 Merck & Co., Inc. 8-Halo-11,12-secoprostaglandins
US4126629A (en) 1975-06-18 1978-11-21 Merck & Co., Inc. Substituted phenoxy-tridecenoic acids/esters
US4087542A (en) 1975-07-09 1978-05-02 Merck & Co., Inc. 2,3-Dihydro-6,7-disubstituted-5-acyl benzofuran-2-carboxylic acids
US4181727A (en) 1975-07-09 1980-01-01 Merck & Co., Inc. 2,3-Dihydro-6,7-disubstituted-5-acyl benzofuran-2-carboxylic acids
US4296122A (en) 1975-07-09 1981-10-20 Merck & Co., Inc. 2,3-Dihydro-6,7-disubstituted-5-(acyl)benzofuran-2-carboxylic acids
US4044153A (en) 1975-08-01 1977-08-23 Merck & Co., Inc. Antiinflammatory 2-aminomethyl-6-trihalomethylphenols
US4203988A (en) 1975-11-12 1980-05-20 Merck & Co., Inc. Pyridinyl ureas and pharmaceutical use
US4029816A (en) 1975-11-25 1977-06-14 Merck & Co., Inc. Substituted 2-aminomethyl-6-iodophenols
US4085211A (en) 1975-12-15 1978-04-18 Merck & Co., Inc. Pyrazinecarboxamides and processes for preparing same
US4070464A (en) 1976-02-19 1978-01-24 Merck & Co., Inc. Method of treating autoimmune diseases
US4066675A (en) 1976-03-22 1978-01-03 Merck & Co., Inc. 9-thia- and oxothia- and 9-dioxothia-11,12-seco-prostaglandins and processes
US4128564A (en) 1976-03-22 1978-12-05 Merck & Co., Inc. 9-Thia- and oxothia- and 9-dioxothia-11,12-seco-prostaglandins
US4029803A (en) 1976-05-03 1977-06-14 Merck & Co., Inc. Method of treatment with 2-iminothiazolidines and thiazolines
US4181661A (en) 1976-05-03 1980-01-01 Merck & Co., Inc. Derivatives of 2-iminothiazolidines and thiazolines
US4059587A (en) 1976-05-24 1977-11-22 Merck & Co., Inc. Certain thiazolidine compounds
US4022794A (en) 1976-05-24 1977-05-10 Merck & Co., Inc. Novel analogs of prostaglandins with 4-oxo-thiazolidinyl nucleus and method of preparation thereof
NL7705652A (nl) 1976-06-15 1977-12-19 Merck & Co Inc 2-imino-3-aminothiazolidinen.
US4025625A (en) 1976-06-15 1977-05-24 Merck & Co., Inc. Imidazothiazines
US4054652A (en) 1976-06-15 1977-10-18 Merck & Co., Inc. Dihydro- and tetrahydro- iminothiazines
US4087526A (en) 1976-07-23 1978-05-02 Merck & Co., Inc. (3-Amino-5-substituted-6-fluoropyrazinoyl or pyrazamido)-guanidines and their derivatives bearing substituents on the guanidino nitrogens
US4111877A (en) 1976-07-29 1978-09-05 Air Products & Chemicals, Inc. Allyl esters of n-alkyl-omega-(alkyleneureido) amic acids and their synthesis and use in aqueous emulsion polymer systems
US4067980A (en) 1976-08-16 1978-01-10 Merck & Co., Inc. Spirobenzoxazinium salts, method of use and compositions thereof as antihypertensive agents
US4085117A (en) 1976-10-18 1978-04-18 Merck & Co., Inc. 6,7-Disubstituted-5-(acyl)benzofuran-2-carboxylic acids
US4100294A (en) 1976-12-06 1978-07-11 Merck & Co., Inc. 5-(Hydroxy (substituted) methyl)-2,3-dihydrobenzo furan-2-carboxylic acid and its derivatives
US4175203A (en) 1976-12-17 1979-11-20 Merck & Co., Inc. Interphenylene 11,12-secoprostaglandins
US4150235A (en) 1976-12-17 1979-04-17 Merck & Co., Inc. Interphenylene 11,12-secoprostaglandins
US4105769A (en) 1977-01-24 1978-08-08 Merck & Co., Inc. Inhibition of indoleamine-N-methyl transferase by 2-iminopyridines
US4087435A (en) 1977-02-17 1978-05-02 Merck & Co., Inc. 8-Aza-9-dioxothiaprostanoic acids
US4115573A (en) 1977-03-04 1978-09-19 Merck & Co., Inc. N-pyrazinecarbonyl-N'-substituted-sulfamoylguanidine and processes for preparing same
US4208413A (en) 1977-03-04 1980-06-17 Merck & Co., Inc. N-Pyrazinecarbonyl-N'-alkoxycarbonyl and N',N"-bis(alkoxycarbonyl)guanidines and processes for preparing same
US4112236A (en) 1977-04-04 1978-09-05 Merck & Co., Inc. Interphenylene 8-aza-9-dioxothia-11,12-secoprostaglandins
US4108859A (en) 1977-06-06 1978-08-22 The Dow Chemical Company Microbicidal (pyridinylamino) alkyl guanidines
US4115402A (en) 1977-06-17 1978-09-19 Merck & Co., Inc. 2,3-Dichloro-4-[(substituted-sulfonyl)-phenoxy]-acetic acids
US4196292A (en) 1977-06-29 1980-04-01 Merck & Co., Inc. 6-Substituted amiloride derivatives
US4133885A (en) 1977-07-18 1979-01-09 Merck & Co., Inc. Substituted naphthyridinones
US4229456A (en) 1977-07-18 1980-10-21 Merck & Co., Inc. Substituted naphthyridinones and processes for their preparations
US4536507A (en) 1977-07-26 1985-08-20 Merck & Co., Inc. Prostaglandin antagonists
US4093728A (en) 1977-08-18 1978-06-06 E. R. Squibb & Sons, Inc. Triazoloisoindoles
US4140776A (en) 1977-09-16 1979-02-20 Merck & Co., Inc. N-pyrazinecarbonyl-N'-acylguanidines
US4130566A (en) 1977-10-27 1978-12-19 Sumitomo Chemical Company, Limited Process for producing 5-carboxy-2-acetylthiophene
US4127584A (en) 1977-11-11 1978-11-28 Merck & Co., Inc. 2,3-Substituted-1,2,5-thiadiazolium salt antimicrobials
US4292430A (en) 1977-11-23 1981-09-29 Merck & Co., Inc. 2,3-Substituted-1,2-isothiazolium salt antimicrobials
US4159279A (en) 1977-11-23 1979-06-26 Merck & Co., Inc. Nuclear substituted 2-hydroxyphenylmethanesulfamic acids
US4267341A (en) 1977-11-23 1981-05-12 Merck & Co., Inc. Process for preparing 2,3-substituted-1,2,-isothiazolium salt antimicrobials
US4166177A (en) 1977-12-27 1979-08-28 Merck & Co., Inc. Substituted 2,2-dioxo-1,2,3-benzoxathiazines
US4145551A (en) 1978-01-09 1979-03-20 Merck & Co., Inc. Pyrazine-2-carbonyloxyguanidines
US4401669A (en) 1978-01-27 1983-08-30 Merck & Co., Inc. 2,3-Dihydro-substituted-5-benzoyl benzofuran-2-carboxylic acids and their use in treating hypertension
US4189496A (en) 1978-02-16 1980-02-19 Merck & Co., Inc. 2,3-Dihydro-5-thienylmethyl and furylmethyl-6-substituted and 6,7-disubstituted-benzofuran-2-carboxylic acid
US4163781A (en) 1978-04-17 1979-08-07 Merck & Co., Inc. 3-Amino-N-[(phosphonoamino)iminomethyl]-6-halopyrazinecarboxamide compounds, compositions and methods of use
US4156005A (en) 1978-06-21 1979-05-22 Merck & Co., Inc. Derivatives of 1,2-benzisoxazoles
US4394515A (en) 1978-06-23 1983-07-19 Merck & Co., Inc. 10,11-Dihydro-11-oxodibenzo[b,f]thiepin compounds
US4263207A (en) 1978-08-01 1981-04-21 Merck & Co., Inc. 10,11-Dihydrodibenzo[b,f][1,4]thiazepine carboxylic acids esters and amides thereof
US4190655A (en) 1978-08-28 1980-02-26 Merck & Co., Inc. Amiloride citrate
US4226867A (en) 1978-10-06 1980-10-07 Merck & Co., Inc. 3,3-Substituted spiro-1,2,4-benzothiadiazines
US4187315A (en) 1978-10-11 1980-02-05 Merck & Co., Inc. N-alkyl(and cycloalkyl)oxamic acid and derivatives as inhibitors of glycolic acid oxidase
US4178386A (en) 1978-10-11 1979-12-11 Merck & Co., Inc. Inhibitors of glycolic acid oxidase
US4207329A (en) 1978-10-11 1980-06-10 Merck & Co., Inc. Derivatives of glycolic and glyoxylic acid as inhibitors of glycolic acid oxidase
US4390537A (en) 1978-11-16 1983-06-28 Merck & Co., Inc. 1-(Substituted-aminoalkoxyphenyl)-2-methylene-1-alkanones, compositions and use
US4342782A (en) 1978-11-16 1982-08-03 Merck & Co., Inc. 1-(Substituted-aminoalkoxyphenyl)-2-methylene-1-alkanones, compositions and use thereof
US4282365A (en) 1978-11-24 1981-08-04 Merck & Co., Inc. Dibenz[b,e]oxepin compounds
US4249021A (en) 1979-02-26 1981-02-03 Merck & Co., Inc. Indanacetic acid compounds
US4246406A (en) 1979-03-27 1981-01-20 Merck & Co., Inc. Heterocyclic substituted pyrazinoylguanidines
US4224447A (en) 1979-03-27 1980-09-23 Merck & Co., Inc. Novel pyrazinecarboxamides and processes for preparing same
US4221790A (en) 1979-04-16 1980-09-09 Merck & Co., Inc. Substituted 2,2-dioxo-1,2,3-benzoxathiazines
US4233452A (en) 1979-05-03 1980-11-11 Merck & Co., Inc. Derivatives of glycolic and glyoxylic acid as inhibitors of glycolic acid oxidase
US4220654A (en) 1979-06-04 1980-09-02 Merck & Co., Inc. Cyclic imidazole cyanoguanidines
US4537902A (en) 1979-06-11 1985-08-27 Merck & Co., Inc. 4-Substituted-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase
US4256758A (en) 1979-06-11 1981-03-17 Merck & Co., Inc. 4-Substituted-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase
US4431660A (en) 1979-06-11 1984-02-14 Merck & Co., Inc. (4'-Biphenylyloxy and-thio-oxy)-3-hydroxy-3-pyrroline-2,5-diones and a method of treating calcium oxalate renal lithiasis therewith
US4237144A (en) 1979-06-21 1980-12-02 Merck & Co., Inc. 2,3-Dihydro-2,6,7-trisubstituted-5-acylbenzofurans
US4237130A (en) 1979-06-21 1980-12-02 Merck & Co., Inc. 2,3-Dihydro-6,7-disubstituted-5-(substituted sulfonyl)benzofuran-2-carboxylic acids
US4291050A (en) 1979-06-21 1981-09-22 Merck & Co., Inc. 6,7-Disubstituted-2 or 2,2-substituted-5-substituted-1-indanones
JPS6034925B2 (ja) 1979-07-31 1985-08-12 帝人株式会社 持続性鼻腔用製剤およびその製造法
US4459422A (en) 1979-08-17 1984-07-10 Merck & Co., Inc. Substituted pyranone inhibitors of cholesterol synthesis
US4710513A (en) 1979-08-17 1987-12-01 Merck & Co., Inc. Substituted pyranone inhibitors of cholesterol synthesis
US4375475A (en) 1979-08-17 1983-03-01 Merck & Co., Inc. Substituted pyranone inhibitors of cholesterol synthesis
US4567289A (en) 1979-08-17 1986-01-28 Merck & Co., Inc. Substituted pyranone inhibitors of cholesterol synthesis
US4298743A (en) 1979-09-11 1981-11-03 Merck & Co., Inc. 4-(Substituted phenyl thiazolyl)-3-hydroxy-3-pyrroline-2,5-diones
US4377588A (en) 1979-09-11 1983-03-22 Merck Sharp & Dohme (I.A.) Corp. 4-(Substituted thiazolyl)-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase
US4379791A (en) 1979-09-11 1983-04-12 Merck & Co., Inc. 4-(Substituted thiazolyl)-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase
US4296237A (en) 1979-09-11 1981-10-20 Merck & Co., Inc. 4-(Pyridyl, piperazinyl and thiazolyl substituted thiazolyl)-3-hydroxy-3-pyrroline-2,5-diones
US4356313A (en) 1979-10-19 1982-10-26 Merck & Co., Inc. [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoic and cycloalkanoic acid esters and their analogs, the parent acids and their salts
US4337354A (en) 1979-10-19 1982-06-29 Merck & Co., Inc. [(5,6,9a-Substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoic and cycloalkanoic acids, their analogs, esters, salts, and derivatives
US4317922A (en) 1979-10-19 1982-03-02 Merck & Co., Inc. [(5,6,9a-Substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoic and cycloalkanoic acids and their analogs, esters, salts and derivatives
US4432992A (en) 1979-11-05 1984-02-21 Merck & Co., Inc. 4-[5(and 4)-Substituted-2-thienyl]-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase
US4448786A (en) 1979-11-05 1984-05-15 Merck & Co., Inc. 4-Naphthyl and substituted naphthyl-3-hydroxy-3-pyrroline-2,5-diones and their use as inhibitors of glycolic acid oxidase
US4349561A (en) 1979-11-05 1982-09-14 Merck & Co., Inc. 4-Substituted-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase
US4342776A (en) 1979-11-05 1982-08-03 Merck & Co., Inc. 4-Substituted-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase
US4260771A (en) 1979-12-20 1981-04-07 Merck & Co., Inc. Interphenylene 9-thia-11-oxo-12-azaprostanoic acid compounds
US4464363A (en) 1979-12-20 1984-08-07 Merck & Co., Inc. Ajuvants for rectal delivery of drug substances
US4428959A (en) 1980-04-04 1984-01-31 Merck & Co., Inc. 4-Alkylsubstituted-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase
US4309540A (en) 1980-05-19 1982-01-05 Merck & Co., Inc. Substituted pyrazinyl-1,2,4-oxadiazoles
US4362724A (en) 1980-05-19 1982-12-07 Merck & Co., Inc. Method of treating edema and hypertension and pharmaceutical composition therefor in which the active ingredient comprises a novel substituted pyrazinyl-1,2,4-oxadiazole and a kaliuretic diuretic
US4356314A (en) 1980-06-30 1982-10-26 Merck & Co., Inc. [5,6,9A-Substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoic and cycloalkanoic acids, their analogs, esters, salts, and derivatives
US4272537A (en) 1980-07-02 1981-06-09 Merck & Co., Inc. 3-Amino-5-substituted-6-halo-N-(4,4-disubstituted-6-substituted-1,3,5-triazin-2-yl)-2-pyrazinecarboxamides
US4317822A (en) 1980-07-02 1982-03-02 Merck & Co., Inc. 3-Amino-5-substituted-6-halo-N-(3,4-dihydro-6-substituted-1,3,5-triazin-2-yl)2-pyrazinecarboxamides
US4277602A (en) 1980-07-02 1981-07-07 Merck & Co., Inc. 3-Amino-5-substituted-6-halo-N-(3,4-dihydro-6-substituted-1,3,5-truazin-2-yl)2-pyrazinecarboxamides
US4465850A (en) 1980-09-02 1984-08-14 Merck & Co., Inc. Treatment of brain injury due to gray matter edema with (indanyloxy) butanoic acids
US4389417A (en) 1980-09-05 1983-06-21 Merck & Co., Inc. Treatment of gray matter edema
US4394385A (en) 1980-11-21 1983-07-19 Merck & Co., Inc. Treatment of gray matter edema
US4316043A (en) 1980-12-19 1982-02-16 Merck & Co., Inc. [(5,6,9a-Substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoic and cycloalkanoic acids and their analogs, esters, salts and derivatives
US4431652A (en) 1980-12-29 1984-02-14 Merck & Co., Inc. 4-Hydroxy-5-substituted-3(2H)-isothiazolone-1,1-dioxide derivatives useful in treating urinary tract calcium oxalate lithiasis
US4336397A (en) 1980-12-29 1982-06-22 Merck & Co., Inc. 2,4-Dioxo-4-substituted-1-butanoic acid derivatives useful in treating urinary tract calcium oxalate lithiasis
US4337258A (en) 1980-12-29 1982-06-29 Merck & Co., Inc. 2,4-Dioxo-4-substituted-1-butanoic acid derivatives useful in treating urinary tract calcium oxalate lithiasis
US4428956A (en) 1980-12-29 1984-01-31 Merck & Co., Inc. 4-Hydroxy-5-substituted-3-(2H)-isothiazolone-1,1-dioxide derivatives useful in treating urinary tract calcium oxalate lithiasis
US4778897A (en) 1981-02-25 1988-10-18 Merck & Co., Inc. 6H-dibenz[b,e][1,4]oxathiepin compounds
US4582842A (en) 1981-02-25 1986-04-15 Merck & Co., Inc. Anti-asthmatic 6H-dibenz-[b,e] [1,4]oxathiepin derivatives, compositions, and method of use therefor
US4454132A (en) 1981-03-16 1984-06-12 Merck & Co., Inc. Pharmaceutical compositions of novel substituted pyrazinyl-1,2,4-oxadiazoles useful in the treatment of edema and hypertension
US4510322A (en) 1981-07-13 1985-04-09 Merck & Co., Inc. Indacrinone having enhanced uricosuric
US4420615A (en) 1981-08-24 1983-12-13 Merck & Co., Inc. Substituted pyridopyrimidines as gastric secretion inhibitors
US4463208A (en) 1981-12-30 1984-07-31 Merck & Co., Inc. Treatment of gray matter edema
US4425337A (en) 1981-12-30 1984-01-10 Merck & Co., Inc. Adjuvants for rectal delivery of drug
US4952582A (en) 1982-01-04 1990-08-28 Beyer Jr Karl H Pyrazinoylguanidine and derivatives thereof having few polar substituents and being useful as hyperuretic agents
US4594349A (en) 1982-01-04 1986-06-10 Beyer Jr Karl H Hyperuretic agents
US4663322A (en) 1982-01-04 1987-05-05 Beyer Jr Karl H Antihypertensive hyperuretic and saluretic agent combinations
US4389393A (en) 1982-03-26 1983-06-21 Forest Laboratories, Inc. Sustained release therapeutic compositions based on high molecular weight hydroxypropylmethylcellulose
US4440740A (en) 1982-04-26 1984-04-03 Merck & Co., Inc. α-Keto aldehydes as enhancing agents of gastro-intestinal drug absorption
US4501729A (en) 1982-12-13 1985-02-26 Research Corporation Aerosolized amiloride treatment of retained pulmonary secretions
JPS6032714A (ja) 1983-08-01 1985-02-19 Teijin Ltd 鼻腔粘膜に適用するための安定化された粉末状薬学的組成物
US4699917A (en) 1983-09-26 1987-10-13 Merck & Co., Inc. Anti-asthmatic tetrazolyl 6H-dibenz-[B,E]-[1,4]-oxathiepin derivatives, compositions, and method of use therefor
US4634717A (en) 1984-05-01 1987-01-06 Merck & Co., Inc. Substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones, useful for treating persons with gray matter edema
US4604403A (en) 1984-05-01 1986-08-05 Merck & Co., Inc. Use of substituted-3(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones for treating grey matter edema
US4680414A (en) 1984-05-01 1987-07-14 Merck & Co., Inc. Substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones
US4605664A (en) 1984-05-01 1986-08-12 Merck & Co., Inc. Use of substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones for treatment of grey matter edema
US4605663A (en) 1984-05-01 1986-08-12 Merck & Co., Inc. Use of substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones, for treatment of grey matter edema
US4596821A (en) 1984-05-01 1986-06-24 Merck & Co., Inc. Treatment of gray matter edema with 3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones
US4604394A (en) 1984-10-01 1986-08-05 Merck & Co., Inc. Antiarrhythmic compositions and method
US4754061A (en) 1985-06-04 1988-06-28 Merck & Co., Inc. Substituted (2,3-dihydro-1-oxo-1H-inden-5-yl)alkanoic acids, their derivatives and their salts
US4579869A (en) 1985-08-02 1986-04-01 Merck & Co., Inc. Substituted [(2,3-dihydro-1-oxo-1H-inden-5-yl)amino]alkanoic acids, their derivatives and their salts
US4604396A (en) 1985-09-26 1986-08-05 Merck & Co., Inc. [(2,3,9,9a-tetrahydro-3-oxo-9a-substituted-1H-fluoren-7-yl)oxy]ethanimidamides and [(2,3,9,9a-tetrahydro-3-oxo-9a-substituted-1H-fluoren-7-yl)oxy]ethanimidic acid hydrazides, their derivatives and their salts
US4654365A (en) 1985-09-26 1987-03-31 Merck & Co., Inc. 2,3-dihydro-5-(3-oxo-2-cyclohexen-1-yl)-2-benzofurancarboxylic acids, and their salts useful in the treatment of brain injury
US4719310A (en) 1985-12-23 1988-01-12 Merck & Co., Inc. Ester and amide substituted (2,3-dihydro-4-(3-oxo-1-cyclohexen-1-yl)phenoxy)alkanoic acids and their salts
US4625047A (en) 1985-12-23 1986-11-25 Merck & Co., Inc. Substituted (2,3-dihydro-4-(3-oxo-1-cyclohexen-1-yl)phenoxy) alkanoic acids, their derivatives and their salts
US4731472A (en) 1986-03-03 1988-03-15 Merck & Co., Inc. (5,6-dichloro-3-oxo-9A-propyl-2,3,9,9A-tetrahydrofluoren-7-yl)alkanoic acids and alkanimidamides
US4835313A (en) 1986-03-03 1989-05-30 Merck & Co., Inc. (5,6-dichloro-3-oxo-9α-propyl-2,3,9,9α-tetrahydrofluoren-7-yl) alkanimidamides
US4777281A (en) 1986-03-03 1988-10-11 Merck & Co., Inc. [3,4-dichloro-6,7,8,8a,9,10-hexahydro-6-oxo-8a-substituted-2-phenanthrenyl)oxy]-alkanoic acids and -ethanimidamides
US4699926A (en) 1986-04-04 1987-10-13 Merck & Co., Inc. Compounds useful in treating sickle cell anemia
US4751244A (en) 1986-04-04 1988-06-14 Merck & Co., Inc. Compounds useful in treating sickle cell anemia
US4731381A (en) 1986-04-04 1988-03-15 Merck & Co., Inc. Method of treating a person for sickle cell anemia
US4731473A (en) 1986-04-04 1988-03-15 Merck & Co., Inc. Compounds useful in treating sickle cell anemia
US4675341A (en) 1986-08-13 1987-06-23 Merck & Co., Inc. [(5,6-dichloro-3-oxo-9a-propyl-2,3,9,9a-tetrahydrofluoren-7-yl)oxy]ethanol and its derivatives
US4937232A (en) 1986-09-15 1990-06-26 Duke University Inhibition of protein kinase C by long-chain bases
US4769370A (en) 1986-09-24 1988-09-06 Merck & Co., Inc. (1,2-dichloro-8-oxo-5a-substituted-5a,6,7,8-tetrahydrodibenzofuran-3-yl)alkanoic acids and alkanimidamides
US4797391A (en) 1986-09-24 1989-01-10 Merck & Co., Inc. ((5,6-dichloro-3-oxo-9,9a-disubstituted-2,3,9,9a-tetrahydrofluoren-7-yl)oxy)alkanoic acids and alkanimidamides
US4731470A (en) 1986-11-03 1988-03-15 Merck & Co., Inc. [(5,6-dichloro-3-oxo-2,9a-alkano-2,3,9,9a-tetrahydro-1H-fluoren-7-yl)oxy]alkanoic acids and alkanimidamides
US4731471A (en) 1986-11-03 1988-03-15 Merck & Co., Inc. (5,6-dichloro-3-oxo-2,3,9,9a-tetrahydrofluoren-7-yl)-alkanoic acids and alkanimidamides bearing novel functional 9a-substituents
US4782073A (en) 1986-12-24 1988-11-01 Merck & Co., Inc. Amides of [(5,6-dichloro-3-oxo-9-alpha-substituted-2,3,9,9-alpha-tetrahydrofluoren-7-yl-oxyl]acetic acids, and pharmaceutical compositions thereof
US4775695A (en) 1987-06-01 1988-10-04 Merck & Co., Inc. Substituted amidinoalkoxy and amidinoalkylamino indanones and salts thereof
US4771076A (en) 1987-06-01 1988-09-13 Merck & Co., Inc. [(2-substituted 1,2-dihydro-1-oxo-1H-inden-5-yl)oxy]alkanesulfonic acids and salts thereof
US5132296A (en) 1987-08-14 1992-07-21 Cherksey Bruce D Membrane NA+ channel protein and related therapeutic compounds
US5242947A (en) 1988-02-10 1993-09-07 New York University Use of polyamines as ionic-channel regulating agents
US4894376A (en) * 1988-02-26 1990-01-16 Trustees Of The University Of Pennsylvania Methods of treating diseases characterized by hyperexcitability of neurons
US4923874A (en) 1988-07-21 1990-05-08 G. D. Searle & Co. Use of 8-azapurin-6-one derivatives for control of hypertension
US5707644A (en) 1989-11-04 1998-01-13 Danbiosyst Uk Limited Small particle compositions for intranasal drug delivery
US5215991A (en) 1990-01-26 1993-06-01 Allergan, Inc. Combination of selective alpha-adrenergic agonists and Na+ /H+ ex
US5449682A (en) 1990-02-13 1995-09-12 Merck & Co., Inc. Angiotensin II antagonists incorporating a substituted benzyl element
US5182299A (en) 1990-03-19 1993-01-26 Brigham And Women's Hospital Treatment of osmotic disturbance with organic osmolytes
KR930701992A (ko) 1990-10-05 1993-09-08 웨인 알.조운즈 환자의 폐에 잔존하는 점액 분비물의 제거 방법
EP0517573A1 (fr) 1991-06-05 1992-12-09 Synthelabo Compositions pharmaceutiques pour le traitement des affections des voies respiratoires
US5292498A (en) 1991-06-19 1994-03-08 The University Of North Carolina At Chapel Hill Method of treating lung disease with uridine triphosphates
US5312820A (en) 1992-07-17 1994-05-17 Merck & Co., Inc. Substituted carbamoyl and oxycarbonyl derivatives of biphenylmethylamines
DE4236237A1 (de) 1992-10-27 1994-04-28 Behringwerke Ag Prodrugs, ihre Herstellung und Verwendung als Arzneimittel
ES2107698T3 (es) 1993-02-20 1997-12-01 Hoechst Ag Benzoilguanidinas sustituidas, procedimiento para su preparacion, su utilizacion como medicamento, como inhibidores del intercambio celular de na+/h+ o como agente de diagnostico, asi como medicamento que las contiene.
US5384128A (en) 1993-03-02 1995-01-24 University Of Alabama Research Foundation Method of and compounds for treatment for cystic fibrosis
US5512269A (en) 1993-06-09 1996-04-30 Burroughs Wellcome, Co. Method of treating retained pulmonary secretions
US6051576A (en) 1994-01-28 2000-04-18 University Of Kentucky Research Foundation Means to achieve sustained release of synergistic drugs by conjugation
AUPM411494A0 (en) 1994-02-25 1994-03-24 Central Sydney Area Health Service Method and device for the provocation of upper or lower airway narrowing and/or the induction of sputum
US5962477A (en) 1994-04-12 1999-10-05 Adolor Corporation Screening methods for cytokine inhibitors
US6190691B1 (en) 1994-04-12 2001-02-20 Adolor Corporation Methods for treating inflammatory conditions
US5538991A (en) 1994-09-14 1996-07-23 Merck & Co., Inc. Endothelin antagonists bearing 5-membered heterocyclic amides
US5618557A (en) 1994-11-22 1997-04-08 E.R. Squibb & Sons, Inc. Prophylactic treatment of allergic contact dermatitis
US5656256A (en) 1994-12-14 1997-08-12 The University Of North Carolina At Chapel Hill Methods of treating lung disease by an aerosol containing benzamil or phenamil
US5908611A (en) 1995-05-05 1999-06-01 The Scripps Research Institute Treatment of viscous mucous-associated diseases
US5635160A (en) 1995-06-07 1997-06-03 The University Of North Carolina At Chapel Hill Dinucleotides useful for the treatment of cystic fibrosis and for hydrating mucus secretions
US5994336A (en) 1995-06-07 1999-11-30 Magainin Pharmaceuticals Inc. Method of inhibiting proliferation of cells by administering an aminosterol compound
US5628984A (en) 1995-07-31 1997-05-13 University Of North Carolina At Chapel Hill Method of detecting lung disease
US5855918A (en) 1995-09-12 1999-01-05 Genentech, Inc. Cystic fibrosis therapy
US6399585B1 (en) 1996-05-15 2002-06-04 Janet E. Larson In Utero treatment of CFTR-related deficiencies
US6015828A (en) 1996-05-31 2000-01-18 Cuppoletti; John Chemical modification of chloride channels as a treatment for cystic fibrosis and other diseases
US6071910A (en) 1996-12-05 2000-06-06 Mayo Foundation For Medical Education And Research Use of agents to treat eosinophil-associated pathologies
KR20010023359A (ko) 1997-08-29 2001-03-26 인스파이어 파마슈티컬즈 폐질환 치료용 우리딘 5'-디포스페이트 및 그의 유사체의용도
US6153187A (en) 1997-09-02 2000-11-28 Insight Strategy & Marketing Ltd. Use of glycosaminoglycans degrading enzymes for management of airway associated diseases
US6159968A (en) 1998-01-15 2000-12-12 University Of Cincinnati Activation of chloride channels for correction of defective chloride transport
US6291514B1 (en) 1998-02-09 2001-09-18 3-Dimensional Pharmaceuticals, Inc. Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors
EP1087777B1 (fr) 1998-05-22 2003-02-19 Inspire Pharmaceuticals, Inc. Dinucleotides therapeutiques et leurs derives
US6294188B1 (en) 1998-07-09 2001-09-25 Aviana Biopharm Inc. Methods involving changing the constitutive and stimulated secretions of the local reproductive system of women
JP4672143B2 (ja) 1998-08-04 2011-04-20 ヤゴテック アーゲー 医薬用エーロゾル製剤
US6136294C1 (en) 1998-09-22 2002-09-24 Aeropharm Technology Inc Amino acid stabilized medical aerosol formulation
US6458338B1 (en) 1998-09-22 2002-10-01 Aeropharm Technology Incorporated Amino acid stabilized medicinal aerosol formulations
EP1143896B1 (fr) * 1998-10-20 2006-12-13 The University of North Carolina at Chapel Hill Methodes pour hydrater des muqueuses nasales
CA2348529A1 (fr) 1998-10-27 2000-05-04 Yale University Conductance de proteines mal repliees dans la voie secretoire
US6926911B1 (en) 1998-12-22 2005-08-09 The University Of North Carolina At Chapel Hill Compounds and methods for the treatment of airway diseases and for the delivery of airway drugs
ATE281837T1 (de) 1999-02-26 2004-11-15 Inspire Pharmaceuticals Verwendung von dinukleotidtriphosphaten, cytidindiphosphaten und adenindiphosphaten zur herstellung einer pharmazeutischen zubereitung zur förderung der schleimauthydratation
US20040195160A1 (en) 1999-07-12 2004-10-07 Marine Desalination Systems, L.L.C. Hydrate-based reduction of fluid inventories and concentration of aqueous and other water-containing products
AU774865B2 (en) 1999-07-19 2004-07-08 University Of North Carolina At Chapel Hill, The Conjugates of sodium channel blockers and methods of using the same
AUPQ344799A0 (en) 1999-10-15 1999-11-11 University Of Sydney, The Treatment of respiratory diseases and infections
US6297226B1 (en) 1999-10-15 2001-10-02 Neotherapeutics, Inc. Synthesis and methods of use of 9-substituted guanine derivatives
JO2178B1 (en) 1999-10-19 2003-04-23 اف . هوفمان لاروش ايه جي Treatment of invasive diseases, using selected anti-PAR materials
US6204270B1 (en) 1999-11-12 2001-03-20 Eyal S. Ron Ophthalmic and mucosal preparations
US6476048B1 (en) 1999-12-07 2002-11-05 Inotek Pharamaceuticals Corporation Substituted phenanthridinones and methods of use thereof
WO2001055390A1 (fr) 2000-01-28 2001-08-02 Human Genome Sciences, Inc. Polynucleotides, polypeptides, et anticorps serpiniques humains
US20040199456A1 (en) 2000-08-01 2004-10-07 Andrew Flint Method and apparatus for explaining credit scores
ATE433962T1 (de) 2000-11-20 2009-07-15 Biovitrum Ab Publ Piperazinylpyrazinverbindungen als antagonisten des serotonin-5-ht2-rezeptors
DE10101440B4 (de) 2001-01-15 2017-10-26 REMS-WERK Christian Föll und Söhne GmbH & Co. Preßzange
US20030135716A1 (en) 2002-01-14 2003-07-17 Gil Vinitzky Method of creating a high performance virtual multiprocessor by adding a new dimension to a processor's pipeline
US6858615B2 (en) * 2002-02-19 2005-02-22 Parion Sciences, Inc. Phenyl guanidine sodium channel blockers
US6858614B2 (en) * 2002-02-19 2005-02-22 Parion Sciences, Inc. Phenolic guanidine sodium channel blockers
US20050227974A9 (en) 2002-08-01 2005-10-13 Euro-Celtique S.A. Aminoalkyl-substituted aryl compounds and their use as sodium channel blockers
US6777721B1 (en) * 2002-11-14 2004-08-17 Altera Corporation SCR device for ESD protection
US6903105B2 (en) 2003-02-19 2005-06-07 Parion Sciences, Inc. Sodium channel blockers
US20050090505A1 (en) * 2003-08-18 2005-04-28 Johnson Michael R. Methods of reducing risk of infection from pathogens
CA2534568A1 (fr) 2003-08-18 2005-03-24 Parion Sciences, Inc. Bloqueurs du canal sodique a base de pyrazinoylguanidine alaphatique
JP2007502829A (ja) * 2003-08-18 2007-02-15 パリオン・サイエンシィズ・インコーポレーテッド 環状ピラジノイルグアニジンナトリウムチャネルブロッカー
US7064129B2 (en) * 2003-08-18 2006-06-20 Parion Sciences, Inc. Capped pyrazinoylguanidine sodium channel blockers
US7745442B2 (en) 2003-08-20 2010-06-29 Parion Sciences, Inc. Methods of reducing risk of infection from pathogens
US20090253714A1 (en) 2003-08-20 2009-10-08 Johnson Michael R Methods of reducing risk of infection from pathogens
US7030717B2 (en) * 2004-05-19 2006-04-18 Soontai Tech Co., Ltd Impedance-matching wave filter
US7375102B2 (en) 2004-06-28 2008-05-20 Amgen Sf, Llc Tetrahydroquinazolin-4(3H)-one-related and tetrahydropyrido[2,3-D]pyrimidin-4(3H)-one-related compounds, compositions and methods for their use
US20090324724A1 (en) 2004-08-18 2009-12-31 Parion Sciences, Inc. Soluble amide & ester pyrazinoylguanidine sodium channel blockers
EP1789049A4 (fr) 2004-08-18 2009-07-22 Michael R Johnson Bloqueurs des canaux sodiques a base d'amide cyclique et d'ester pyrazinoylguanidine
AU2005277443A1 (en) * 2004-08-18 2006-03-02 Johnson, Michael R Aliphatic amide and ester pyrazinoylguanidine sodium channel blockers
US7399766B2 (en) * 2004-08-18 2008-07-15 Parion Sciences, Inc. Soluble amide & ester pyrazinoylguanidine sodium channel blockers
JP4964469B2 (ja) 2005-01-14 2012-06-27 ガジック・テクニカル・エンタープライゼス 磁気ヘッド及びディスクをテストするための真空チャック・スピンスタンド
US20070021439A1 (en) 2005-07-25 2007-01-25 Parion Sciences, Inc. Methods of reducing risk of infection from pathogens with soluble amide and ester pyrazinoylguanidine sodium channel blockers
US7807834B2 (en) 2005-08-03 2010-10-05 Parion Sciences, Inc. Capped pyrazinoylguanidine sodium channel blockers
GB0526244D0 (en) 2005-12-22 2006-02-01 Novartis Ag Organic compounds
GB0526240D0 (en) 2005-12-22 2006-02-01 Novartis Ag Organic compounds
CA2652072A1 (fr) 2006-05-12 2007-11-22 Vertex Pharmaceuticals Incorporated Compositions de n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoleine-3-carboxamide
WO2007146867A2 (fr) 2006-06-09 2007-12-21 Parion Sciences Inc. Bloqueurs de canaux sodiques pyrazinoylguanidine aliphatiques dotés d'une activité agoniste bêta
PT2035004E (pt) 2006-06-09 2012-11-21 Parion Sciences Inc Bloqueadores dos canais de sódio de pirazinoilguanidona substituída com fenilo que possuem actividade agonista beta
US20110195973A1 (en) 2006-06-09 2011-08-11 Parion Sciences, Inc. Cyclic substituted pyrazinoylguanidine sodium channel blockers possessing beta agonist activity
MX2009002602A (es) 2006-09-07 2009-05-28 Parion Sciences Inc Metodos para aumentar la hidratacion mucosa y el despeje mucoso mediante tratamiento con bloqueadores de canal de sodio y osmolitos.
CN101534813A (zh) 2006-09-07 2009-09-16 帕里昂科学公司 通过使用钠通道阻断剂和渗透调节剂的治疗来增加粘膜水化和粘液清除的方法
EP2059239A4 (fr) * 2006-09-07 2010-07-07 Parion Sciences Inc Hydratation de muqueuse et clairance de muqueuse améliorées par traitement avec bloqueurs de canal sodique et osmolytes
US20080293740A1 (en) 2007-04-03 2008-11-27 Parion Sciences, Inc. Method of treating acid-sensing ion channel mediated pain, cough suppression, and central nervous system disorders
WO2008124491A1 (fr) 2007-04-03 2008-10-16 Parion Sciences, Inc. Composes de pyrazinoylguanidine destines a etre utilises en tant que modulateurs de gout
EP2332933A1 (fr) 2007-05-07 2011-06-15 Novartis AG Inhibiteurs du canal sodique épithélial
CA2702094C (fr) 2007-10-10 2018-05-01 Parion Sciences, Inc. Administration d'osmolytes par canule nasale
NZ585789A (en) 2007-12-10 2012-03-30 Novartis Ag Pyrazine-2-carboxamide derivatives to treat diseases mediated by blockade of the epithelial sodium channel
AU2009246799B2 (en) 2008-02-26 2014-02-27 Parion Sciences, Inc. Poly aromatic pyrazinoylguanidine sodium channel blockers
US8261047B2 (en) 2008-03-17 2012-09-04 Freescale Semiconductor, Inc. Qualification of conditional debug instructions based on address
US8664228B2 (en) 2008-05-13 2014-03-04 Novartis Ag 3,5-diamino-6-chloro-pyrazine-2-carboxylic acid derivatives and their use as epithelial sodium channel blockers for the treatment of airway diseases
EA201001848A1 (ru) 2008-06-10 2011-08-30 Новартис Аг Производные пиразина в качестве блокаторов эпителиальных натриевых каналов
US20100074881A1 (en) * 2008-07-11 2010-03-25 Parion Sciences, Inc. Multiple nebulizer systems
KR20110074916A (ko) 2008-10-23 2011-07-04 버텍스 파마슈티칼스 인코포레이티드 N-(4-(7-아자비시클로[2.2.1]헵탄-7-일)-2-(트리플루오로메틸)페닐)-4-옥소-5-(트리플루오로메틸)-1,4-디히드로퀴놀린-3-카르복스아미드의 고체 형태
US8247436B2 (en) 2010-03-19 2012-08-21 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF
WO2011156355A1 (fr) 2010-06-09 2011-12-15 Kainos Medicine, Inc. Procédé de production de sels de phénylguanidine et de leurs intermédiaires
KR20120017648A (ko) 2010-08-19 2012-02-29 삼성전자주식회사 디스플레이장치와, 디스플레이 패널의 구동방법
ES2633177T3 (es) 2011-06-27 2017-09-19 Parion Sciences, Inc. Dipéptido química y metabólicamente estable que presenta una potente actividad bloqueadora de los canales de sodio
AR086745A1 (es) 2011-06-27 2014-01-22 Parion Sciences Inc 3,5-diamino-6-cloro-n-(n-(4-(4-(2-(hexil(2,3,4,5,6-pentahidroxihexil)amino)etoxi)fenil)butil)carbamimidoil)pirazina-2-carboxamida
EA201990616A3 (ru) 2012-05-29 2019-12-30 Парион Сайэнс, Инк. Дендримероподобные аминоамиды, обладающие активностью блокаторов натриевых каналов, для лечения сухости глаз и других заболеваний слизистых оболочек
WO2014036445A2 (fr) 2012-08-31 2014-03-06 Johnson Michael R Nouveaux agents mucolytiques
JP6263193B2 (ja) 2012-11-15 2018-01-17 バイエル ファーマ アクチエンゲゼルシャフト スルホキシイミン基を含んでいる5−フルオロ−n−(ピリジン−2−イル)ピリジン−2−アミン誘導体
JP6392242B2 (ja) 2012-12-17 2018-09-19 パリオン・サイエンシィズ・インコーポレーテッド 粘膜への水分付与が不十分であることが好都合である疾患の治療に有用なクロロ−ピラジンカルボキサミド誘導体
NZ709197A (en) 2012-12-17 2020-06-26 Parion Sciences Inc 3,5-diamino-6-chloro-n-(n-(4-phenylbutyl)carbamimidoyl) pyrazine-2- carboxamide compounds
HK1223561A1 (zh) 2013-08-23 2017-08-04 帕里昂科学公司 二巯基化物类粘液溶解剂
US9102633B2 (en) 2013-12-13 2015-08-11 Parion Sciences, Inc. Arylalkyl- and aryloxyalkyl-substituted epithelial sodium channel blocking compounds
US20150376145A1 (en) 2014-06-30 2015-12-31 Parion Sciences, Inc. Stable sodium channel blockers

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3313813A (en) * 1962-10-30 1967-04-11 Merck & Co Inc (3-amino-5, 6-disubstituted-pyrazinoyl) guanidines
US3573306A (en) * 1969-03-05 1971-03-30 Merck & Co Inc Process for preparation of n-substituted 3,5-diamino-6-halopyrazinamides

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
BICKING ET AL.: "Pyrazine diuretics. I. N-amidino-3-amino-6-halopyrazine carboxamides", J. MED. CHEM., vol. 8, no. 5, 1965, pages 638 - 642, XP002967520 *
EPAND ET AL.: "Reversal of intrinsic multidrug resistance in Chinese hamster ovary cells by amiloride analogs", BRITISH JOURNAL OF CANCER, vol. 63, no. 2, 1991, pages 247 - 251, XP002967521 *

Cited By (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8431579B2 (en) 2003-08-18 2013-04-30 Parion Sciences, Inc. Capped pyrazinoylguanidine sodium channel blockers
US8008494B2 (en) 2004-08-18 2011-08-30 Parion Sciences, Inc. Soluble amide and ester pyrazinoylguanidine sodium channel blockers
US8022210B2 (en) 2004-08-18 2011-09-20 Parion Sciences, Inc. Soluble amide and ester pyrazinoylguanidine sodium channel blockers
US7956059B2 (en) 2004-08-18 2011-06-07 Parion Sciences, Inc. Aliphatic amide and ester pyrazinoylguanidine sodium channel blockers
US10752597B2 (en) 2011-06-27 2020-08-25 Parion Sciences, Inc. 3,5-diamino-6-chloro-N—(N-(4-(4-(2-(hexyl(2,3,4,5,6-pentahydroxyhexyl)amino)ethoxy)phenyl)butyl)carbamimidoyl)pyrazine-2-carboxamide
US9586910B2 (en) 2011-06-27 2017-03-07 Parion Sciences, Inc. 3,5-diamino-6-chloro-N-(N-(4-(4-(2-(hexyl(2,3,4,5,6-pentahydroxyhexyl)amino)ethoxy)phenyl)butyl)carbamimidoyl)pyrazine-2-carboxamide
US11578042B2 (en) 2011-06-27 2023-02-14 Parion Sciences, Inc. 3,5-diamino-6-chloro-N-(N-(4-(4-(2-(hexyl(2,3,4,5,6-pentahydroxyhexyl)amino)ethoxy)phenyl)butyl)carbamimidoyl)pyrazine-2-carboxamide
US9593084B2 (en) 2012-12-17 2017-03-14 Parion Sciences, Inc. Chloro-pyrazine carboxamide derivatives with epithelial sodium channel blocking activity
US10071970B2 (en) 2012-12-17 2018-09-11 Parion Sciences, Inc. Chloro-pyrazine carboxamide derivatives with epithelial sodium channel blocking activity
US10246425B2 (en) 2012-12-17 2019-04-02 Parion Sciences, Inc. 3,5-diamino-6-chloro-N-(N-(4-phenylbutyl)carbamimidoyl) pyrazine-2-carboxamide compounds
US9695134B2 (en) 2012-12-17 2017-07-04 Parion Sciences, Inc. 3,5-diamino-6-chloro-N-(n-(4-phenylbutyl)carbamimidoyl)pyrazine-2-carboxamide compounds
US9957238B2 (en) 2013-12-13 2018-05-01 Parion Sciences, Inc. Arylalkyl-and aryloxyalkyl-substituted epithelial sodium channel blocking compounds
US10233158B2 (en) 2013-12-13 2019-03-19 Parion Sciences, Inc. Arylalkyl- and aryloxyalkyl-substituted epithelial sodium channel blocking compounds
US9586911B2 (en) 2013-12-13 2017-03-07 Parion Sciences, Inc. Arylalkyl- and aryloxyalkyl-substituted epthelial sodium channel blocking compounds

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